Laboratório de Pesquisa Em Micologia Aplicada (LPMA), Universidade Federal Do Rio Grande Do Sul, Rua São Luís 152, Porto Alegre, 90470-440, Brazil.
Programa de Pós-Graduação Em Ciências Farmacêuticas, Universidade Federal Do Rio Grande Do Sul (UFRGS), Av. Ipiranga 2752, Porto Alegre, 90610-000, Brazil.
Curr Microbiol. 2024 Nov 4;81(12):441. doi: 10.1007/s00284-024-03960-x.
The current global scenario presents us with a growing increase in infections caused by fungi, referred to by specialists in the field as a "silent epidemic", aggravated by the limited pharmacological arsenal and increasing resistance to this therapy. For this reason, drug repositioning and therapeutic compound combinations are promising strategies to mitigate this serious problem. In this context, this study investigates the antifungal activity of the non-toxic, low-cost and widely available cationic polyelectrolyte Poly(diallyldimethylammonium chloride) (PDDA), in combination with different antifungal drugs: systemic (amphotericin B, AMB), topical (clioquinol, CLIO) and oral (nitroxoline, NTX). For each combination, different drug:PDDA ratios were tested and, through the broth microdilution technique, the minimum inhibitory concentration (MIC) of these drugs in the different ratios against clinically important Candida species strains was determined. Overall, PDDA combinations with the studied drugs demonstrated a significant increase in drug activity against most strains, reaching MIC reductions of up to 512 fold for the fluconazole resistant Candida krusei (Pichia kudriavzevii). In particular, the AMB-PDDA combination 1:99 was highly effective against AMB-resistant strains, demonstrating the excellent profile of PDDA as an adjuvant/association in novel antifungal formulations with outdated conventional drugs.
当前的全球形势呈现出由真菌引起的感染不断增加的趋势,该领域的专家称之为“无声的流行”,这种情况因药理学武器库有限和对这种治疗方法的耐药性增加而加剧。因此,药物再定位和治疗化合物组合是缓解这一严重问题的有前途的策略。在这种情况下,本研究调查了非毒性、低成本且广泛可用的阳离子聚电解质聚(二烯丙基二甲基氯化铵)(PDDA)与不同抗真菌药物联合的抗真菌活性:全身性(两性霉素 B,AMB)、局部(氯己定,CLIO)和口服(硝呋太尔,NTX)。对于每种组合,测试了不同的药物:PDDA 比例,并通过肉汤微量稀释技术,确定了这些药物在不同比例下对临床重要的念珠菌属菌株的最低抑菌浓度(MIC)。总体而言,与研究药物的 PDDA 组合显示出对大多数菌株的药物活性显著增加,对氟康唑耐药的近平滑念珠菌(毕赤酵母)的 MIC 降低高达 512 倍。特别是 AMB-PDDA 组合 1:99 对 AMB 耐药菌株非常有效,证明了 PDDA 作为一种佐剂/联合物在具有过时传统药物的新型抗真菌制剂中的出色表现。